TAN-67 [Ligand Id: 9567] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL327745 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Displacement of [3H]-Naltrindole from DOR (unknown origin) | B | 6.67 | pKi | 215.8 | nM | Ki | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Displacement of [3H]-Naltrindole from DOR (unknown origin) | B | 6.02 | pEC50 | 961.2 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480] |
| ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480] |
| ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670] |
| δ receptor/Delta-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in mouse whole brain membranes | B | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307] |
| ChEMBL | inhibition of [3H]DADLE binding to delta-opioid receptor of mouse brain homogenates | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2967-2972 |
| GtoPdb | Bioassay using mouse vas deferens. | - | 8.44 | pIC50 | 3.65 | nM | IC50 | Drug Des Discov (2001) 17: 325-30 [PMID:11765135] |
| δ receptor/Delta-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]DADLE from delta opioid receptor in rat cerebellum membrane | B | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480] |
| ChEMBL | Displacement of [3H]DADLE from delta opioid receptor in rat cerebrum membranes | B | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670] |
| κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]-Diprenorphine from KOR (unknown origin) | B | 5.56 | pKi | 2762 | nM | Ki | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Displacement of [3H]-Diprenorphine from KOR (unknown origin) | B | 4.95 | pEC50 | 11140 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| κ receptor/Kappa-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Binding affinity against Kappa opioid receptor using [3H]U-69593 radioligand in mouse brain homogenates | B | 6.51 | pKi | 312 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2967-2972 |
| Kappa-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes | B | 6.14 | pKi | 732.5 | nM | Ki | Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum | B | 6.14 | pKi | 732.45 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480] |
| ChEMBL | Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum membranes | B | 6.14 | pKi | 732.45 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307] |
| MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1] | ||||||||
| GtoPdb | Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR). | - | 5.74 | pEC50 | 1820 | nM | EC50 |
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]; Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]; Drug Des Discov (2001) 17: 325-30 [PMID:11765135] |
| ChEMBL | Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay | F | 6.37 | pEC50 | 426.58 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay | F | 6.54 | pEC50 | 290 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay | F | 6.54 | pEC50 | 288.4 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]-DAMGO from MOR (unknown origin) | B | 5.81 | pKi | 1557 | nM | Ki | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Displacement of [3H]-DAMGO from MOR (unknown origin) | B | 5.68 | pEC50 | 2109 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| μ receptor/Mu-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes | B | 6.55 | pKi | 284.14 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6302-6305 [PMID:20850307] |
| ChEMBL | Inhibition of [3H]DAMGO from mouse brain homogenate Mu opioid receptor | B | 7.22 | pKi | 59.6 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2967-2972 |
| μ receptor/Mu-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat cerebellum membrane | B | 6.55 | pKi | 284.14 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2792-2795 [PMID:19362480] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat cerebrum membranes | B | 6.55 | pKi | 284.1 | nM | Ki | Bioorg Med Chem (2012) 20: 949-961 [PMID:22197670] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
